For research use only. Not for therapeutic Use.
iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research[1].
iHCK-37 (5.0-20 μM; 24 hours) exhibits a potent in vitro antiproliferative activity. The dose (μM) for growth inhibition (GI50) is 5.0-5.8 μM for AML cell lines (HL60, KG1a and U937) and 9.1-19.2 μM for chronic myeloid leukemia cell lines (HEL and K562)[2].iHCK-37 (3-9 μM; plus Erythropoietin) leads to a decrease in ERK, AKT and P70S6K phosphorylation of in lentivirus HCK silenced K562 and U937 cell lines[2].iHCK-37 (3-9 μM) results in a decrease of p-HCK, p-ERK, p-AKT, p-70S6 in the cell line KG1a (AML/CD34+), in a dose-dependent manner[2].
| Catalog Number | I044445 |
| CAS Number | 516478-09-4 |
| Synonyms | N-(2-morpholin-4-ylphenyl)-2-[[2-(2-phenylethyl)-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-4-yl]sulfanyl]acetamide |
| Molecular Formula | C30H32N4O2S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C30H32N4O2S2/c35-27(31-23-11-5-6-12-24(23)34-16-18-36-19-17-34)20-37-29-28-22-10-4-7-13-25(22)38-30(28)33-26(32-29)15-14-21-8-2-1-3-9-21/h1-3,5-6,8-9,11-12H,4,7,10,13-20H2,(H,31,35) |
| InChIKey | YBVMBFMOYYGDEM-UHFFFAOYSA-N |
| SMILES | C1CCC2=C(C1)C3=C(S2)N=C(N=C3SCC(=O)NC4=CC=CC=C4N5CCOCC5)CCC6=CC=CC=C6 |
| Reference | [1]. Cristina Tintori, et al. Identification of Hck inhibitors as hits for the development of antileukemia and anti-HIV agents. ChemMedChem. 2013 Aug;8(8):1353-60. [2]. Fernanda Marconi Roversi, et al. Hematopoietic cell kinase (HCK) is a potential therapeutic target for dysplastic and leukemic cells due to integration of erythropoietin/PI3K pathway and regulation of erythropoiesis: HCK in erythropoietin/PI3K pathway. Bi |
